[go: up one dir, main page]

MA34652B1 - HETEROARYLATES AND USES THEREOF - Google Patents

HETEROARYLATES AND USES THEREOF

Info

Publication number
MA34652B1
MA34652B1 MA35882A MA35882A MA34652B1 MA 34652 B1 MA34652 B1 MA 34652B1 MA 35882 A MA35882 A MA 35882A MA 35882 A MA35882 A MA 35882A MA 34652 B1 MA34652 B1 MA 34652B1
Authority
MA
Morocco
Prior art keywords
heteroarylates
compounds
pi3k
mtor
inflammatory
Prior art date
Application number
MA35882A
Other languages
French (fr)
Inventor
Brian S Freeze
Masaaki Hirose
Hong Myung Lee
Todd B Sells
Zhan Shi
Leo R Takaoka
Stepan Vyskocil
Tianlin Xu
Original Assignee
Millennium Pharm Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=45938970&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MA34652(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Millennium Pharm Inc filed Critical Millennium Pharm Inc
Publication of MA34652B1 publication Critical patent/MA34652B1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/78Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Rheumatology (AREA)
  • Biophysics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Transplantation (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

CETTE INVENTION CONCERNE DES COMPOSÉS DE FORMULE I-A OU I-B : DANS LESQUELS HY, G1, G2, R2, R12, W1, W2, N, ET LE CYCLE A SONT TELS QUE DÉCRITS DANS LA DESCRIPTION. LES COMPOSÉS SONT DES INHIBITEURS DE PI3K ET/OU MTOR ET SONT PAR CONSÉQUENT UTILES POUR TRAITER DES TROUBLES PROLIFÉRATIFS, INFLAMMATOIRES, OU CARDIOVASCULAIRES.THIS INVENTION CONCERNS COMPOUNDS OF FORMULA I-A OR I-B: IN WHICH HY, G1, G2, R2, R12, W1, W2, N, AND CYCLE A ARE AS DESCRIBED IN THE DESCRIPTION. THE COMPOUNDS ARE INHIBITORS OF PI3K AND / OR MTOR AND ARE THEREFORE USEFUL IN TREATING PROLIFERATIVE, INFLAMMATORY, OR CARDIOVASCULAR DISORDERS.

MA35882A 2010-10-13 2013-05-06 HETEROARYLATES AND USES THEREOF MA34652B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US39251510P 2010-10-13 2010-10-13
PCT/US2011/056135 WO2012051410A2 (en) 2010-10-13 2011-10-13 Heteroaryls and uses thereof

Publications (1)

Publication Number Publication Date
MA34652B1 true MA34652B1 (en) 2013-11-02

Family

ID=45938970

Family Applications (1)

Application Number Title Priority Date Filing Date
MA35882A MA34652B1 (en) 2010-10-13 2013-05-06 HETEROARYLATES AND USES THEREOF

Country Status (24)

Country Link
US (2) US8765746B2 (en)
EP (1) EP2627181A4 (en)
JP (1) JP2013542941A (en)
KR (1) KR20140091462A (en)
CN (1) CN103237450A (en)
AR (1) AR083450A1 (en)
AU (1) AU2011316016A1 (en)
BR (1) BR112013009166A2 (en)
CA (1) CA2814688A1 (en)
CL (1) CL2013001009A1 (en)
CO (1) CO6801713A2 (en)
CR (1) CR20130204A (en)
DO (1) DOP2013000082A (en)
EA (1) EA201390539A1 (en)
EC (1) ECSP13012621A (en)
IL (1) IL225607A0 (en)
MA (1) MA34652B1 (en)
MX (1) MX2013004003A (en)
PE (1) PE20141044A1 (en)
PH (1) PH12013500723A1 (en)
SG (1) SG189396A1 (en)
TW (1) TW201307309A (en)
UY (1) UY33671A (en)
WO (1) WO2012051410A2 (en)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009094224A1 (en) 2008-01-25 2009-07-30 Millennium Pharmaceuticals, Inc. Thiophenes and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors
US9139589B2 (en) 2009-01-30 2015-09-22 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US9090601B2 (en) 2009-01-30 2015-07-28 Millennium Pharmaceuticals, Inc. Thiazole derivatives
US8796314B2 (en) 2009-01-30 2014-08-05 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
WO2012021611A1 (en) 2010-08-11 2012-02-16 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
TW201217365A (en) 2010-08-11 2012-05-01 Millennium Pharm Inc Heteroaryls and uses thereof
EP2603216A4 (en) 2010-08-11 2013-12-18 Millennium Pharm Inc Heteroaryls and uses thereof
CN103467481B (en) * 2012-06-07 2016-08-31 上海汇伦生命科技有限公司 Dihydropyridine compounds, a combination thereof thing, preparation method and purposes
US9586949B2 (en) 2015-02-09 2017-03-07 Incyte Corporation Aza-heteroaryl compounds as PI3K-gamma inhibitors
US10065963B2 (en) 2015-11-06 2018-09-04 Incyte Corporation Heterocyclic compounds as PI3K-γ inhibitors
US20170190689A1 (en) 2016-01-05 2017-07-06 Incyte Corporation Pyridine and pyridimine compounds as pi3k-gamma inhibitors
US10138248B2 (en) 2016-06-24 2018-11-27 Incyte Corporation Substituted imidazo[2,1-f][1,2,4]triazines, substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-b]pyridazines and substituted imidazo[1,2-a]pyrazines as PI3K-γ inhibitors
WO2019027368A1 (en) * 2017-07-31 2019-02-07 Agency For Science, Technology And Research Method of preparing stapled peptides
WO2019079469A1 (en) 2017-10-18 2019-04-25 Incyte Corporation Condensed imidazole derivatives substituted by tertiary hydroxy groups as pi3k-gamma inhibitors
CR20250050A (en) 2018-09-05 2025-03-19 Incyte Corp Crystalline forms of a phosphoinositide 3-kinase (pi3k) inhibitor
CN110041349B (en) * 2019-05-15 2021-06-01 湖南科技大学 Spiro-containing dihydropyrimidine derivative and preparation method and application thereof
TWI879771B (en) 2019-06-06 2025-04-11 大陸商和記黃埔醫藥(上海)有限公司 Tricyclic compounds and their use

Family Cites Families (93)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE581861A (en) 1958-08-20
US3852293A (en) 1972-06-21 1974-12-03 Uniroyal Inc 4-phenyl-2-(3-pyridyl)-thiazole carboxamides
US3821384A (en) 1972-10-06 1974-06-28 Uniroyal Inc Pharmaceutical compositions containing a4-aryl-2-(3-pyridyl)thiazole and methods of using same
DE3021590A1 (en) 1980-06-09 1981-12-17 Hoechst Ag, 6000 Frankfurt 4-HALOGEN-5- (HALOGENMETHYL-PHENYL) -OXAZOLE DERIVATIVES, A METHOD FOR THE PRODUCTION THEREOF AND THEIR RADIO-SENSITIVE MEASURES
DD275870A1 (en) 1988-09-27 1990-02-07 Univ Leipzig PROCESS FOR THE PREPARATION OF DIFFERENTLY SUBSTITUTED 3-AMINOTHIOPHENE-4-CARBONITRILES IN 5-POSITION
PH27357A (en) 1989-09-22 1993-06-21 Fujisawa Pharmaceutical Co Pyrazole derivatives and pharmaceutical compositions comprising the same
AU6966696A (en) 1995-10-05 1997-04-28 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
US6268308B1 (en) 1996-08-27 2001-07-31 Syngenta Crop Protection, Inc. Herbicidal S-substituted 1,2,4,6-thiatriazines
JPH1087490A (en) 1996-09-10 1998-04-07 Sagami Chem Res Center Interleukin-6 production inhibitor, bone resorption inhibitor, antiosteoporotic agent, and thiazole compound
PT853083E (en) 1997-01-06 2001-12-28 Pfizer COMPOSITION OF PYRIDILFURANE AND PYRIDYLTHOPHENE AND ITS PHARMACEUTICAL UTILIZATION
ES2167882T3 (en) 1997-04-24 2002-05-16 Dow Agrosciences Llc 3- (REPLACED PHENYL) -5- (TIENIL OR FURIL) -1,2,4-PESTICIDE TRIAZOLS.
EP1097147A4 (en) 1998-07-10 2001-11-21 Merck & Co Inc Novel angiogenesis inhibitors
DE19858192A1 (en) 1998-12-17 2000-06-21 Aventis Cropscience Gmbh 4-Trifluoromethyl-3-oxazolylpyridines, process for their preparation, compositions containing them and their use as pesticides
CO5170501A1 (en) 1999-04-14 2002-06-27 Novartis Ag USEFUL REPLACED BLUES FOR THE TREATMENT OF DISEASES MEDIATED BY TNFa eIL-1 AND DISEASES OF THE OSEO METABOLISM
EP1251848B1 (en) 2000-01-18 2004-06-23 Vertex Pharmaceuticals Incorporated Gyrase inhibitors and uses thereof
US6642227B2 (en) 2001-04-13 2003-11-04 Vertex Pharmaceuticals Incorporated Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
ATE402164T1 (en) 2001-04-26 2008-08-15 Eisai R&D Man Co Ltd NITROGEN CONTAINING COMPOUND HAVING A CONDENSED RING AND PYRAZOLYL GROUP AS A SUBSTITUENT AND MEDICAL COMPOSITION THEREOF
US7405235B2 (en) 2001-05-04 2008-07-29 Paratek Pharmaceuticals, Inc. Transcription factor modulating compounds and methods of use thereof
CN100502863C (en) 2001-08-13 2009-06-24 詹森药业有限公司 2,4, 5-trisubstituted thiazole derivatives and their anti-inflammatory activity
DE60228098D1 (en) 2001-09-05 2008-09-18 Smithkline Beecham Plc PYRIDIN-SUBSTITUTED FURANDERIVATES AS RAF-KINASE INHIBITORS
JP2005532983A (en) 2001-09-26 2005-11-04 バイエル・フアーマシユーチカルズ・コーポレーシヨン 3-Pyridyl or 4-isoquinolinyl thiazole as C17,20 lyase inhibitor
US20040198773A1 (en) 2001-09-26 2004-10-07 Barry Hart Substituted 3-pyridyl oxazoles as c17,20 lyase inhibitors
AR039555A1 (en) 2001-11-08 2005-02-23 Upjohn Co N, N'-SUBSTITUTED DERIVATIVES OF 1,3-DIAMINO-2-HYDROXIPROPANE
MXPA05001544A (en) 2002-08-08 2005-04-19 Smithkline Beecham Corp Thiophene compounds.
EP1534680B1 (en) 2002-08-14 2012-02-22 Pharmaco Investments, Inc. Prenylation inhibitors and methods of their synthesis and use
US20050004122A1 (en) 2002-08-14 2005-01-06 Brown Bradley B. Prenylation inhibitors containing dimethylcyclobutane and methods of their synthesis and use
TW200519106A (en) 2003-05-02 2005-06-16 Novartis Ag Organic compounds
US6984652B2 (en) 2003-09-05 2006-01-10 Warner-Lambert Company Llc Gyrase inhibitors
JP2007519753A (en) 2004-01-30 2007-07-19 スミスクライン ビーチャム コーポレーション Compound
WO2005095386A1 (en) 2004-03-30 2005-10-13 Chiron Corporation Substituted thiophene derivatives as anti-cancer agents
WO2006078287A2 (en) 2004-05-06 2006-07-27 Plexxikon, Inc. Pde4b inhibitors and uses therefor
GB0423653D0 (en) * 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
JP2008524329A (en) 2004-12-21 2008-07-10 メルク エンド カムパニー インコーポレーテッド Mitotic kinesin inhibitor
CA2594477C (en) 2005-01-21 2016-07-12 Astex Therapeutics Limited Pharmaceutical compounds
GB0503962D0 (en) 2005-02-25 2005-04-06 Kudos Pharm Ltd Compounds
CN1834095B (en) 2005-03-18 2011-04-20 中国科学院上海药物研究所 Nonnucleoside antivirus inhibitor, its preparation method and use
KR20070120963A (en) 2005-03-21 2007-12-26 일라이 릴리 앤드 캄파니 Imidazopyridazine Compound
GB0508471D0 (en) * 2005-04-26 2005-06-01 Celltech R&D Ltd Therapeutic agents
GB0508472D0 (en) 2005-04-26 2005-06-01 Glaxo Group Ltd Compounds
DE102005000046A1 (en) 2005-04-28 2006-11-02 Voith Patent Gmbh Papermaking machine press section, for the production of super calender paper, has a center roller forming two press nips where the paper passes through with a smooth blanket
EP1910307A1 (en) 2005-06-27 2008-04-16 Exelixis, Inc. Pyrazole based lxr modulators
WO2007043400A1 (en) 2005-10-07 2007-04-19 Kissei Pharmaceutical Co., Ltd. Nitrogenated aromatic heterocyclic compound and pharmaceutical composition comprising the same
JP2007197324A (en) 2006-01-23 2007-08-09 Toray Ind Inc 2,4,5-substituted-1,3-azole derivative
HRP20130058T1 (en) 2006-01-24 2013-02-28 Eli Lilly & Company Indole sulfonamide modulators of progesterone receptors
US7504513B2 (en) 2006-02-27 2009-03-17 Hoffman-La Roche Inc. Thiazolyl-benzimidazoles
NZ572202A (en) 2006-03-27 2012-05-25 Nerviano Medical Sciences Srl Pyridyl- and pyrimidinyl-substituted pyrrole-, thiophene- and furane-derivatives as kinase inhibitors
BRPI0710874A2 (en) 2006-04-26 2012-02-14 Hoffmann La Roche thienopyrimidine compounds, processes for producing said compounds, pharmaceutical compositions containing them, kit, product, and uses of the compounds
US20090076009A1 (en) 2006-05-03 2009-03-19 Arnould Jean-Claude Retired Thiazole derivatives and their use as anti-tumour agents
CN101484447A (en) 2006-05-23 2009-07-15 沃泰克斯药物股份有限公司 Thiophene-carboxamides useful as inhibitors of protein kinases
WO2007138110A2 (en) 2006-06-01 2007-12-06 Devgen N.V. Compounds that interact with ion channels, in particular with ion channels from the kv family
WO2008001076A1 (en) * 2006-06-26 2008-01-03 Ucb Pharma S.A. Fused thiazole derivatives as kinase inhibitors
US20080021217A1 (en) 2006-07-20 2008-01-24 Allen Borchardt Heterocyclic inhibitors of rho kinase
US20100143499A1 (en) 2006-07-24 2010-06-10 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
EP2385050A1 (en) 2006-08-14 2011-11-09 Schering Corporation A process for preparing a substituted oxazole
MX2009002046A (en) 2006-08-24 2009-03-06 Astrazeneca Ab Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders.
US20090093452A1 (en) 2006-08-24 2009-04-09 Pfizer Inc. Pyrrole, Thiophene, Furan, Imidazole, Oxazole, and Thiazole Derivatives
CA2662000C (en) 2006-09-20 2013-01-08 Eli Lilly And Company Thiophene pyrazolopyrimidine compounds
JP2010511682A (en) 2006-12-04 2010-04-15 アストラゼネカ アクチボラグ Antibacterial polycyclic urea compounds
WO2008083070A1 (en) 2006-12-29 2008-07-10 Neurogen Corporation Crf1 receptor ligands comprising fused bicyclic heteroaryl moieties
GB0701426D0 (en) 2007-01-25 2007-03-07 Univ Sheffield Compounds and their use
CA2677264C (en) 2007-02-02 2021-11-30 Baylor College Of Medicine Compositions and methods for the treatment of metabolic disorders
UY30892A1 (en) 2007-02-07 2008-09-02 Smithkline Beckman Corp AKT ACTIVITY INHIBITORS
US8420690B2 (en) 2007-02-07 2013-04-16 Glaxosmithkline Llc Inhibitors of Akt activity
CL2008001234A1 (en) 2007-04-30 2008-09-22 Genentech Inc COMPOUNDS DERIVED FROM NITROGEN HETEROCICLES, INHIBITORS OF APOPTOSIS PROTEINS; AND USE IN THE TREATMENT OF CANCER.
GB0709031D0 (en) 2007-05-10 2007-06-20 Sareum Ltd Pharmaceutical compounds
WO2008157273A1 (en) 2007-06-14 2008-12-24 Smithkline Beecham Corporation Chemical compounds
WO2009006577A2 (en) 2007-07-03 2009-01-08 The Regents Of The University Of Michigan Compositions and methods for inhibiting ezh2
US8067613B2 (en) 2007-07-16 2011-11-29 Abbott Laboratories Benzimidazole poly(ADP ribose)polymerase inhibitors
CA2704711C (en) 2007-09-24 2016-07-05 Genentech, Inc. Thiazolopyrimidine p13k inhibitor compounds and methods of use
WO2009040730A2 (en) 2007-09-24 2009-04-02 Actelion Pharmaceuticals Ltd Pyrrolidines and piperidines as orexin receptor antagonists
WO2009049028A1 (en) 2007-10-09 2009-04-16 Targegen Inc. Pyrrolopyrimidine compounds and their use as janus kinase modulators
WO2009094224A1 (en) 2008-01-25 2009-07-30 Millennium Pharmaceuticals, Inc. Thiophenes and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors
TW200940537A (en) 2008-02-26 2009-10-01 Astrazeneca Ab Heterocyclic urea derivatives and methods of use thereof
PL2276767T3 (en) 2008-03-31 2014-09-30 Genentech Inc Benzopyran and benzoxepin pi3k inhibitor compounds and methods of use
GB0805818D0 (en) 2008-03-31 2008-04-30 Ucb Pharma Sa Therapeutic agents
AU2009260782B2 (en) 2008-06-19 2014-12-11 Millennium Pharmaceuticals, Inc. Thiophene or thiazole derivatives and their use as PI3K inhibitors
JP2011525931A (en) 2008-06-26 2011-09-29 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Inhibitor of Akt activity
GB0812309D0 (en) 2008-07-03 2008-08-13 Ucb Pharma Sa Therapeutic agents
US8420695B2 (en) 2008-07-09 2013-04-16 Merck Sharp & Dohme Corp. Inhibitors of janus kinases
JP5698666B2 (en) 2008-08-04 2015-04-08 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. Oxazole derivatives useful as inhibitors of FAAH
KR20110098908A (en) 2008-11-11 2011-09-02 엑스커버리 홀딩 컴퍼니 엘엘씨 PI3K / MTOR Kinase Inhibitor
GB0820819D0 (en) 2008-11-13 2008-12-24 Sareum Ltd Pharmaceutical compounds
WO2010080873A1 (en) 2009-01-08 2010-07-15 Glaxo Group Limited Oxazoles as modulators of chemokine receptors
US9090601B2 (en) 2009-01-30 2015-07-28 Millennium Pharmaceuticals, Inc. Thiazole derivatives
US8796314B2 (en) 2009-01-30 2014-08-05 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US9139589B2 (en) 2009-01-30 2015-09-22 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
MX2011012037A (en) 2009-05-13 2012-02-28 Amgen Inc Heteroaryl compounds as pikk inhibitors.
US20110021531A1 (en) 2009-07-27 2011-01-27 Chobanian Harry Oxazole derivatives useful as inhibitors of faah
JP2012254939A (en) 2009-10-07 2012-12-27 Astellas Pharma Inc Oxazole compound
WO2012021611A1 (en) 2010-08-11 2012-02-16 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
EP2603216A4 (en) 2010-08-11 2013-12-18 Millennium Pharm Inc Heteroaryls and uses thereof
TW201217365A (en) 2010-08-11 2012-05-01 Millennium Pharm Inc Heteroaryls and uses thereof
WO2013096642A1 (en) 2011-12-23 2013-06-27 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof

Also Published As

Publication number Publication date
CA2814688A1 (en) 2012-04-19
JP2013542941A (en) 2013-11-28
US20150148334A1 (en) 2015-05-28
SG189396A1 (en) 2013-05-31
WO2012051410A2 (en) 2012-04-19
EP2627181A2 (en) 2013-08-21
IL225607A0 (en) 2013-06-27
AU2011316016A1 (en) 2013-05-30
US20120214794A1 (en) 2012-08-23
MX2013004003A (en) 2013-10-01
EP2627181A4 (en) 2014-03-19
PH12013500723A1 (en) 2017-08-23
UY33671A (en) 2012-04-30
KR20140091462A (en) 2014-07-21
BR112013009166A2 (en) 2016-07-26
US8765746B2 (en) 2014-07-01
DOP2013000082A (en) 2013-10-31
CR20130204A (en) 2013-09-03
PE20141044A1 (en) 2014-09-07
EA201390539A1 (en) 2013-09-30
ECSP13012621A (en) 2013-07-31
TW201307309A (en) 2013-02-16
CN103237450A (en) 2013-08-07
CO6801713A2 (en) 2013-11-29
WO2012051410A3 (en) 2012-07-26
CL2013001009A1 (en) 2013-08-30
AR083450A1 (en) 2013-02-27

Similar Documents

Publication Publication Date Title
MA34652B1 (en) HETEROARYLATES AND USES THEREOF
MA34797B1 (en) HETEROARYLES AND THEIR USES
MX2015005015A (en) HETEROARILO PDE4 INHIBITORS.
EA201491412A1 (en) CONNECTIONS FOR THE TREATMENT OF SPINAL MUSCULAR ATROPHY
EA201491766A1 (en) CONNECTIONS FOR THE TREATMENT OF SPINAL MUSCULAR ATROPHY
EA201492056A1 (en) Pyrimidinyl inhibitors of tyrosine kinase
BR112015001695A2 (en) heteroaryl and heterocycle compounds, compositions and methods
EA201170052A1 (en) DERIVATIVES OF TIOPHENE OR THIAZOLE AND THEIR APPLICATION AS PI3K INHIBITORS
EA201400735A1 (en) DERIVATIVES ALPHA-AMINO BORONIC ACID, SELECTIVE INHIBITORS IMMUNOPROTEASOMA
EA201400412A1 (en) SUBSTITUTED BENZILINDAZOLES FOR USE AS BUB1 INHIBITORS KINAZES FOR THE TREATMENT OF HYPERPROLIFERATIVE DISEASES
EA201390609A1 (en) HIDANTOIN DERIVATIVES USEFUL AS KV3-CHANNEL INHIBITORS
MA37756A1 (en) New compounds diazaspirocycloalkane and azaspirocycloalkane
CR20140229A (en) NEW BICYCLIC DERIVATIVES OF DIHIDROISOQUINOLIN-1-ONA
IN2014KN02601A (en)
MX2010002732A (en) F1f0-atpase inhibitors and related methods.
EA201491303A1 (en) CONDENSED TETRA- OR PENTACYCLIC DIHYDRODIAZEPINOCARBAZOLONES AS PARPS INHIBITORS
EA201290642A1 (en) CONNECTIONS AND METHODS
PH12013501255A1 (en) Anti-notch1 antibodies
EP2331093A4 (en) COMPOUNDS, COMPOSITIONS AND METHODS FOR REDUCING TOXICITY AND FOR TREATING OR PREVENTING DISEASES
EA201590552A1 (en) AMINOHINOLINES AS KINASE INHIBITORS
MA34968B1 (en) ASYMMETRIC UREA AND MEDICAL USES THEREOF
MA37625A1 (en) Derivatives of the prodrug type of (e) -N-methyl-n - ((3-methylbenzofuran-2-yl) methyl) -3- (7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridine -3-yl) acrylamide
MA39170B1 (en) Serine / threonine kinase inhibitory compounds for their uses in the treatment of cancer
EP2519512A4 (en) The present invention relates to the field of N1-acyl-5-fluoropyrimidinones and their derivatives and the use of its compounds as fungicides
EA201690523A1 (en) TRIAZOLOPIRIDIN, COMPOSITIONS AND METHODS OF THEIR APPLICATION